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AKI603
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AKI603
CAS No. : 1432515-73-5
MCE 站:AKI603
产品活性:AKI603 是一种极光激酶 A (AurA) 抑制剂,其 IC50 值为 12.3 nM,被开发用于克服白血病中 BCR-ABL-T315I 耐药性突变。AKI603 对白血病细胞具有很强的抗增殖活性。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:Aurora Kinase
In Vitro: AKI603 (0.039-0.6 μM; 48 hours) extensively inhibits proliferation of leukemia cells.
AKI603 (0.039-0.6 μM; 48 hours) significantly inhibits the phosphorylation of AurA in NB4, K562, and Jurkat cell lines in a dose-dependent manner while the level of total AurA protein is not changed.
AKI603 inhibits the proliferation and colony formation of imatinib resistant CML cells.
AKI603 (0.3-0.6 μM; 48 hours) inhibits cell proliferation and colony formation capacities in imatinib-resistant CML cells by inducing cell cycle arrest with polyploidy accumulation.
Inhibition of AurA by AKI603 induces leukemia cell senescence in both BCR-ABL wild type and T315I mutation cells.
AKI603 exhibits inhibitory activities on breast cancer cell proliferation, such as SUM149 (IC50=2.04), BT549 (IC50=0.86), MCF-7 (IC50=0.97), MCF-7-Epi (IC50=21.01), Sk-br-3 (IC50=0.73), MDA-MB-231 (IC50=3.49), MDA-MB-453 (MTT, IC50=0.18; Cell counting, IC50=0.19), MDA-MB-468 (MTT, IC50=0.15; Cell counting, IC50=0.17).
In Vivo: AKI603 (12.5-25?mg/kg; i.p.; every 2 days; for 14 days) abrogates the growth of xenografted KBM5-T315I cells in nude mice.
AKI603 exhibits moderate oral bioavailability (rat 28.7%) and Cmax (rat 202.4 μg/L) following oral administration (rat 25 mg/kg).
AKI603 exhibits terminal elimination half-life (rat 8.9 h) following intravenous administration (rat 2.5 mg/kg).
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Kinase Inhibitor Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Anti-Breast Cancer Compound Library | Anti-Blood Cancer Compound Library | AT9283 | KW-2449 | PF-03814735 | ZM-447439 | SNS-314 mesylate | CCT 137690 | SCH-1473759 hydrochloride | NU6140 | Aurora kinase inhibitor-2 | Tripolin A | Aurora B inhibitor 1 | Aurora inhibitor 1
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